HYDROCORTISON
Composition:
Hydrocortisoni natrii succinas (Hydrocortisonum natrium 21-succinicum) 133.7 mg
(= 100 mg hydrocortisonum) of the substance in a phial.
Indication Group:
Hormone of the glucocorticoid group.
ATC : H02AB09
Characteristics:
Soluble salt of natural human glucocorticoid of hydrocortison, suitable for parenteral use; mineralocorticoidal effect is in comparison with other preparations of this group relatively high, it starts very quickly and it weakens early. High doses (megadoses) have own pharmaceutical effect with vasodilatation in the area of microcirculation and with improvement of tissue perfusion; they are stabilisers of membranes. Medium and small doses have especially immunological, substitutional, antifibrinoplastic and anti-inflammatory effect.
Pharmacokinetic Properties:
Active substance is metabolised in liver, it is excreted in urine; it penetrates placental barrier.
Indication:
Megadoses of Hydrocortison ICN are indicated during toxico-infective shock namely by gramnegative strains; during a protracted shock with serious dysfunction of microcirculation, during thyreotoxic crisis, malignant hyperthermia syndrome, after a bite by highly poisonous snakes; they are administered in a single dose during acute conditions, at most diphasically; they will not suppress intrinsic production of cortisol.
Medium doses of Hydrocortison ICN are indicated during absolute or relative insufficiency of the adrenal cortex: Addison’s disease with crisis, a condition after a both-sides adrenalectomy, an increased load of organism during a simultaneous depletion of its intrinsic reserves, e.g. during an operative procedure, a serious injury, a chronic sepsis. Hydrocortison ICN also secures the organism substitutionally after an extirpation of adrenal tumour during Cushing’s disease, after a hypophysectomy; during myasthenia gravis, asthmatic condition, bronchial asthma, lupus erythematodes etc. It is further indicated during an acute myocardial infarction, laryngeal edema (post-radiation or post-intubation), brain edema, virus polyneuritis and polyradiculoneuritis. The preparation can be also administered topically in this indication – e.g. in a spray to the mucosa of larynx. After this administration, the penetration of antibiotics into the so-called third space (encapsulated focuses and alike) is improved.
Small doses are indicated mostly after a long-term administration during myasthenia gravis, during chronic respiratory insufficiency with the spastic component and peribronchitis, during conditions after hepatitis, after a long-term artificial ventilation of lungs and tracheotomy, during a bioclimatic sensitivity in exposed conditions. Parenterally administered Hydrocortison ICN can be effective also in cases where peroral treatment with the same preparation fails.
THIOPENTHAL
Composition:
Active substance: thiopentalum natricum 500 mg or 1 g in 1 vial
Adjuvant: natrii carbonas
Indication Group:
General anaesthetic
ATC : N01AF03
Characteristic:
Shortly efective barbiturate intravenous anaesthetic, which passes through hemato-encephalic barrier easily; it lacks analgesic and relaxant effect, it has anticonvulsive effect; falling asleep is fast and calm, waking up is gradual; the anaesthesia does not proceed according to the classic Guedel’s scheme.
Pharmacokinetic Data:
After i.v. administration, the effective concentration in brain is formed approximately after 30 seconds; it is bound in a large share to the blood-plasma proteins. The short clinical effect of a single dose is given by redistribution.Degradation through disulphuration by hepatic enzymes proceeds to oxybarbiturate of a medium-long effect. Repeated doses cause effect prolongation; biological half-life is 3-6 hours (but also 16 hours). Elimination half-life is 11.5 hours.
The active substance penetrates placental barrier; it passes in breast milk, breast feeding must be interrupted for 24 hours after a Thiopental anaesthesia.
Pharmacodynamic Data:
Because of its high lipophylity Thiopental penetrates easily the hemato-encephalic barrier and suppresses almost simultaneously subcortex and cortex of brain. The depth of anaesthesia is dependant on the dose, its effect progresses from cortical level up to the level of medulla oblongata.
Indication:
Introduction into total anaesthesia; short-term performances approximately up to 15 minutes in total anaesthesia; incision, probatory excision, revision of uterine cavity, painful bandages, repositions, electroshocks and alike; it is necessary to supplement the preparation with suitable analgesics or with inhalation of a mixture of oxygen and nitrogen monoxide for painful procedures; it is a part of supplemented total anaesthesia.
It is possible to use it also rectally for basal anaesthesia of small children; it is possible to use it for management of spasms during tetanus, eclampsia, epilepsy, overdose and toxic reaction to local anaesthetics.
Thiopental can be selectively used for brain-metabolism suppression after neurotraumas, respectively after hypoxial insults of brain during a continuing infusion, titrated according to EEG. Dose in a continual infusion is between 1-3 mg/kg/hour.
SUCCINYLCHOLINJODID
Composition:
Suxamethonii iodidum 100 or 250 mg of dried substance in 1 injection vial.
Indication group:
Muscular myorelaxans.
ATC : M03AB01
Characteristics:
Very shortly acting muscular relaxant of depolarising type; it relaxes excellently especially muscles of larynx. It belongs to the group of quarterly ammonium bases.
Suxamethonium is bound to postjunctional acetylcholine receptors of myoneural junctions of striated muscles. It causes depolarisation in their functional area by means of acetylcholine-effect imitation. The effect is manifested by muscular contractions followed by relaxation, lasting till the degradation of suxamethonium by plasmatic cholinesterase.
Pharmacokinetic data:
90% of the administered substance is degraded by plasmatic cholinesterase. The first metabolite – succinylmonocholin – has a weak non-depolarising curarimimetic effect; in the following phase of biotransformation it is degraded to choline and succinic acid. Approximately 10% is excreted in unchanged form in urine; the effect ends within 3-5 minutes. After a single-dose administration the active substance penetrates placental barrier and comes into breast milk in a slight quantity.
Indication:
Tracheal intubation, especially for so-called lightning intubation; performances demanding short-term relaxation; non-sanguineous repositions, divulsion of anal sphincter, facilitation suture peritonea, laryngospasm, relaxation during caesarian section till the foetus extraction, cardioversion and alike.
CHLORAMPHENICOL
Composition:
Chloramphenicoli natrii succinas (Chloramphenicolum succinicum natricum) 1.38 g
(= 1 g of the base) in 1 phial for the preparation of the injection solution.
Indication group:
Antibiotic.
ATC : J01BA01
Characteristic:
Synthetic wide-spectrum bacteriostatic antibiotic the use of which is reserved only for serious infections caused by sensitive microbes, that can not be treated with other, less toxic antibiotics.
Chloramphenicol is very well effective for salmonellae, yersiniae, haemophilus, bordetelia, gonococcus, meningococcus and anaerobic microorganisms; brucells, francisels, leptospires and treponems, corynebacteria, listeria, bacillus of anthrax, actinomyces, pleuropneumonia-like organisms and chlamydia and rickettsia are also well sensitive. Most (60-80% of strains) gramnegative rods (Escherichia coli, Enterobacter Klebsiella, Citrobacter, Proteus, Providencia, Shigella and alike) and enterococcus are further sensitive to chloramphenicol.
Even if streptococcus and pneumococcus are very well sensitive to chloramphenicol, penicillin preparations are preferred. Staphylococcus are also mostly sensitive to chloramphenicol (about 70% of strains), but better therapeutical results can usually be accomplished by anti-staphylococcus antibiotics (erythromycin, oxacillin). Indol-positive strains protea, Enterobacter spp., Citrobacter spp., Pseudomonas aeruginosa and mycobacteria are mostly resistent.
Pharmacokinetic data:
After a parenteral administration, the ester sodium chloramphenicolsuccinate is hydrolysed by tissue enzymes and the liberated chloramphenicol forms levels approximately equally high as after an administration of an equal dose per os.
Chloramphenicol penetrates into cerebrospinal fluid and measurable concentrations are in bronchial secreta, lungs, pleural liquid, in bile, peritoneum, ascites, in saliva, milk, ocular fluid and in bones. It reaches in tissues approximately 50% of the serum concentration. It is eliminated in urine, only about 5-15% of chloramphenicol is eliminated in biologically active form, the rest is eliminated in the form of glucuronides; the amount of free chloramphenicol is however sufficient to create sufficiently active concentrations in urine; during 8 hours after the administration 50-65% of total administered amount is eliminated in urine. Biological half-life of chloramphenicol is 2.5-5 hours, during anuria up to 7 hours, during liver insufficiency 5-13 hours. It is not dialysed during haemodialysis and during peritoneal dialysis. The active substance penetrates placental barrier, concentrations in umbilical blood are a bit lower than in blood of the mother. It comes into breast milk (a possibility to develop icterus in sucklings).
Indication:
Typhoid fever and typhus, salmonellosis with a septic course, meningitis, epiglottitis, pertussis and parapertussis, serious infections with an occurrence of aerobic and anaerobic flora (pulmonary, abdominal, gynaecologic and alike)and other infections whose infective agent is sensitive only to chloramphenicol.